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Chopra A.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Nov 14 [updated 2012 Dec 27].


Development of Alzheimer's disease (AD) has been attributed to neurodegeneration as a result of the neuronal overexpression, secretion, and deposition of the neurotoxic amyloid β (Aβ) fragment of the Aβ protein precursor in the brain (1). No specific treatment for AD is currently available, and clinicians are increasingly focused on developing ways to either prevent or delay the formation of Aβ plaques in the brain of AD patients (2). In addition, several hundred clinical trials approved by the United States Food and Drug Administration have been completed or are in progress to develop drugs for the prevention, onset delay, or treatment of AD. Early detection of Aβ plaques by noninvasive techniques such as positron emission tomography (PET) are often used to identify individuals who are prone to develop the disease and to monitor the efficacy of drugs used to treat or delay onset of the disease (3). The 11C-labeled Pittsburgh compound B ([11C]PIB) is the most commonly used PET tracer for the detection of Aβ plaques, but the short half-life of 11C (20.4 min) restricts the use of this label to clinical facilities that have the capability to generate the probe on site (3). Some 18F-labeled compounds (half-life of 18F is ~110 min) have also been generated for the visualization of Aβ plaques, but these labeled compounds usually show low specificity toward the plaques (3). Investigators have synthesized some 18F-labeled PIB analogs, such as [18F]BAY94-9172 (4) and [18F]flutemetamol (2-{3-[18F]Fluoro-4-(methylamino)phenyl}-1,3-benzothiazol-6-ol) (5), earlier known as [18F]GE067 (6), and are evaluating these probes for the detection and diagnosis of AD in the clinic. Flutemetamol is a thioflavin T derivative of PIB and bears 18F-fluorine on the 3' position of the parent molecule (7). The biodistribution and PET imaging of Aβ plaques with [18F]flutemetamol have been investigated in rodents (8), healthy human volunteers (5, 6), and patients with mild cognitive impairment (7) and AD (5, 6).

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